CONICET | Buscador de Institutos y Recursos Humanos

Emulsions are gaining increasing interest to be applied as drug delivery systems. The main goal of this work was the formulationof an oil/water nutraceutical emulsion (NE) for oral administration, enriched in omega 3 (3) and omega 6 (6), and able to encapsulaterisperidone (RISP), an antipsychotic drug widely used in the treatment of autism spectrum disorders (ASD). RISP has low solubility inaqueous medium and poor bioavailability because of its metabolism and high protein binding. Coadministration of 3, 3, and vitaminE complexed with RISP might increase its bioavailability and induce a synergistic effect on the treatment of ASD. Here, we developed aneasy and quick method to obtain NEs and then optimized them. The best formulation was chosen after characterization by particle size,defects of the oil-in-water interface, zeta potential (ZP), and in vitro drug release. The formulation selected was stable over time, with aparticle size of around 3 m, a ZP lower than −20 mV and controlled drug release. To better understand the biochemical properties ofthe formulation obtained, we studied in vitro toxicity in the Caco-2 cell line. After 4 h of treatment, an increase in cellular metabolismwas observed for all RISP concentrations, but emulsions did not change their metabolic rate, except at the highest concentration withoutdrug (25 g/mL), which showed a signiﬁcant reduction in metabolism respect to the control. Additionally, locomotor activity and heartrate in zebraﬁsh were measured as parameters of in vivo toxicity. Only the highest concentration (0.625 g/mL) showed a cardiotoxiceffect, which corresponds to the decrease in spontaneous movement observed previously. As all the materials contained in the formulationswere US FDA approved, the NE selected would be good candidate for clinical trials.